Antimalarial activity of new gossypol derivatives |
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Authors: | Valérie Razakantoanina Nguyen Kim Phi Phung Ginette Jaureguiberry |
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Institution: | (1) FR 63, CNRS Laboratoire de Biologie parasitaire, Museum National d'Histoire Naturelle, 61, rue Buffon, 75005 Paris, France e-mail: jauregui@mnhn.fr Tel.:+33-140-793504; Fax: +33-140-793499, FR;(2) Faculty of Sciences, International University, Ho Chi Minh City, Viet Nam, VN |
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Abstract: | Gossypol, a disesquiterpene extracted from cotton seeds, is known to inhibit strongly the Plasmodium falciparum lactate dehydrogenase, but its high toxicity has stopped any antimalarial drug development. A series of Schiff's bases was
synthesized from gossypol by modification of the aldehyde groups responsible for its toxicity. A total of 13 compounds showing
low cytotoxicity were then selected and were compared with gossypol for activity against 2 chloroquine-resistant strains of
P. falciparum (PFB, FCB1). These in vitro activities were evaluated using an isotope-based drug-susceptibility semiautomated microdilution
test followed by determination of IC50 values (50% inhibitory concentration). In all, 12 of the 13 compounds tested were active; 3 of them displayed antimalarial
activity comparable with that of gossypol itself.
Received: 27 November 1999 / Accepted: 28 January 2000 |
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